Artemisia annua
Qinghao
ARTEMISIAE ANNUAE HERBA
Qinghao
ARTEMISIAE ANNUAE HERBA
This product is the dry aboveground part of Artemisia annua L., a Compositae plant. In autumn, the flowers are cut when they are in full bloom. The old stems are removed and dried in the shade.
[character] the stem of this product is cylindrical, with many branches in the upper part, 30 ~ 80cm long, 0.2 ~ 0.6cm in diameter, yellow green or brown yellow surface, with longitudinal edges; The texture is slightly hard and easy to break, and there is marrow in the middle of the section. The leaves are alternate, dark green or brownish green, curly and fragile, and the complete ones are three pinnate deep lobes after flattening, with lobes and lobules rectangular round or long oval, and both sides are covered with short hairs. The smell is special and the taste is slightly bitter.
[identification] take 3G of this product powder, add 50ml of petroleum ether (60 ~ 90 ℃), heat and reflux for 1 hour, filter, evaporate the filtrate, add 30ml of n-hexane to dissolve the residue, shake and extract with 20% acetonitrile solution for three times, 10ml each time, combine the acetonitrile solution, evaporate to dryness, add 0.5ml of ethanol to dissolve the residue, and use it as the test solution. In addition, take artemisinin reference substance and add ethanol to make a solution containing 1mg per 1ml as the reference substance solution. According to the test of thin-layer chromatography (general rule 0502), suck 5 μ l of each of the above two solutions, dot them on the same silica gel G thin-layer plate respectively, use petroleum ether (60 ～ 90 ℃) - diethyl ether (4:5) as the developing agent, develop, take out, air dry, spray with 10% sulfuric acid ethanol solution of 2% vanillin, heat at 105 ℃ until the spots develop clearly, and check under ultraviolet light (365nm). In the chromatogram of the test sample, fluorescent spots of the same color appear at the corresponding positions of the chromatogram of the control sample.
[inspection] the moisture content shall not exceed 14.0% (the second method of general rule 0832).
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[extract] determined according to the cold leaching method under the alcohol soluble extract determination method (general rule 2201), using absolute ethanol as solvent, it shall not be less than 1.9%.
Decoction pieces
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[nature, taste and meridian tropism] bitter, pungent and cold. Return to liver and gallbladder channels.
[functions and indications] clearing deficiency heat, eliminating bone steaming, relieving summer heat, intercepting malaria, and eliminating jaundice. It is used for warming evil to injure Yin, night heat and early cooling, yin deficiency fever, bone steaming fever, summer evil fever, malaria cold and heat, damp heat jaundice.
[usage and dosage] 6-12g, rear lower.
[storage] store in a cool and dry place.
2、 Chemical constituents of Artemisia annua
The aerial part contains terpenoids:artemisinin（qinghaosu. Artemi-sinin,arteannuin）， , artemisinin A,arteannuin A）， Qinghaosu II, artemisinin B,arteannuin B）， Artemisinin III is hydrogenated artemisinin, deoxyartemisinin (Qinghaosu III, hydroartemisinin,de-oxyartemisinin）， Qinghaosu Ⅳ, qinghaosu Ⅴ, qinghaosu Ⅵ, artemisinin C, arteannuin g, an isomer of artemisinin B, ,Artemisinic acid（qinghao acid，artemisic acid,artemisinic acid,arteannuic acid）， , Friedelin and friedelan 3 β -ol, etc; Flavonoids; ,Vitexin（casticin）， Cirsiliol, 5,3-dihydroxy-6,7,4-trimethoxyflavone, 5,7,3,4-tetrahydroxy-dimethoxyflavone, cirsiliol, tamarixetin, rhamnetin, quercetin-3-methylether, cirsimarin, rhamnoci trin, chrysoeriol, 5, 2,4-trihydroxy-6,7,5-trimethoxyflavone (5,2,4-trihydroxy-6,2,4-trihydroxy-6,7, 5-trimethoxyflavone）， 5,7,8,3-tetrahydroxy-3,4-dimethoxyflavone, quercetagen-3,4-dimethyl,Kaempferol（kaempferol），quercetin （quercetin），Luteolin（luteolin）， Patuletin, quercetin-3-rutinoside, luteolin-7-o-glyco-side, kaempferol-3-o-glucopferol-3-o-glucoside, quercetin-3-o-glucoside, patuletin-3-o-glucoside, and 6-methoxykaempferol-3- O-glycoside (6-methoxykaempferol-3-o-glucoside); ;Scopoletin Pavilion（scopoletin）， Coumarin, 6,8-dimethoxy-7-hydroxycoumarin, 5,6-dimethoxy-7-hydroxycoumarin and scoparon, etc; ,Linalool（linalool）， Isoborneol,α - terpineol（α-terpineol），Borneol（borneol）， Camphene, myrcene, limonene, γ - terpineol, Bornyl isovalerate, γ - cadinene, ξ - picturene, α - elemene, β - elemene, γ - elemene [20],salicylic acid(salicylic acid), β - Terpinene, α - thujene, 4-terpineol, 4-terpingyl acetate, andLinalyl acetate(linlayl acetate) et al; Others:palmitic acid（palmitic acid），Stigmasterol（stigmasterol），β - sitosterol（β-sitosterol）， Aurantiamide acetate, 5-nonadecylresorcinol-3-o-methylether, nonacosanol, 2-methyltriacosan-8-one-23-ol, hentriacontanol triaconta noate, 2,29-dimethyltriacontane, annuadi epoxide), Ponticae poxide and β -glucosidase Ⅰ with relative molecular weights of 150000 and 100000, respectivelyβ - glycosidaseII et al.
3、 Pharmacological effects of Artemisia annua
1. antimalarial effect: the neutral part of Artemisia annua ether extract and its dilute alcohol extract have significant antimalarial effect on mouse malaria, monkey malaria and human malaria. The in vivo test showed that artemisinin had killing effect on the inner phase of Plasmodium falciparum erythrocytes, but had no effect on the outer phase of erythrocytes and pre erythrocytes. Artemisinin can rapidly inhibit the maturation of protozoa. The antimalarial effect of artemether emulsion is better than that of reduced artemisinin sodium succinate, which is an ideal dosage form for the treatment of dangerous malaria. Artesunate 2.5, 5, 10, 15mg / kg, twice a day for three consecutive days, applied externally on the skin, has different degrees of efficacy in the treatment of monkey malaria. 5、10mg／kg， Twice a day for 10 consecutive days, external application of the skin can turn the monkey malaria negative. The antimalarial effect can be improved by adding an appropriate amount of Azone. . In vitro tests showed that artemisinin could significantly inhibit the growth of P. falciparum clones and had a direct killing effect. The IC50 of artemisinin, artemether and chloroquine against Plasmodium falciparum were 75.2, 29.4 and 43.2nmol / L, respectively. Artemisinin ester sodium has inhibitory effect on six isolates of Plasmodium falciparum, including chloroquine resistant strains.
2. antibacterial effect: Artemisia annua water decoction has strong antibacterial effect on Staphylococcus epidermidis, catarrhalis, Bacillus anthracis, diphtheria bacilli, and also has certain inhibitory effect on Staphylococcus aureus, Pseudomonas aeruginosa, dysentery bacilli, stem tuberculosis, etc. When the concentration of Artemisia annua volatile oil is 0.25%, it has antibacterial effect on all dermatophytes, and when the concentration is 1%, it has bactericidal effect on all dermatophytes. Artemisinin has the effect of anti influenza virus. Sodium artesunate has certain antibacterial effects on Staphylococcus aureus, Shigella flexneri, Escherichia coli, catarrhalis, and culm paratyphi A and B. Sitosterol and stigmasterol in Artemisia annua also have antiviral effects.
3. antiparasitic effect: Artemisia annua ether extract, dilute alcohol extract and artemisinin have significant antimalarial effect on mouse malaria, monkey malaria and human malaria. . The electron microscopic observation showed that artemisinin mainly acted on the membrane phase structure of the Plasmodium parasite's erythrocyte inner phase clone, first acting on the food color membrane, surface membrane and mitochondrial membrane, followed by the nuclear membrane and endoplasmic reticulum. In addition, it also affects the chromosomes in the nucleus. Due to the changes in the food vesicle membrane, the early stage of the malaria parasite's uptake of nutrients is blocked, so that the malaria parasite rapidly undergoes amino acid starvation, forms autophagic vacuoles, and is continuously discharged from the body, causing a large loss of the vacuole plasma, the internal structure disintegration and death. Artemisinin has high curative effect on vivax malaria, falciparum malaria and falciparum malaria in chloroquine resistant areas, and has the characteristics of rapid antipyretic and negative conversion time of protozoa. It is especially suitable for rescuing dangerous malaria, but has a high recurrence rate. In addition, Artemisia annua has anti schistosomiasis and Leptospira effects.
4. antipyretic effect: Artemisia annua injection prepared by distillation method has obvious antipyretic effect on rabbits caused by the triple vaccine of hundred, white and tetanus. Artemisia annua and honeysuckle prescription, the Qingyin injection prepared by distillation method, has a more significant antipyretic effect on the domestic immunity to the fever caused by the triple vaccine of typhoid fever, paratyphoid fever A and B than the single Artemisia annua injection. Its cooling characteristics are rapid and lasting, which is better than the control group of Bupleurum and Antongding Injection. Honeysuckle and Artemisia annua have synergistic antipyretic effect.
5. immune effect: the immune effect of artemisinin was observed by four immune indexes, including mouse foot pad test, lymphocyte transformation test, rabbit epidemic specific rose test and hemolytic plaque test. It was found that artemisinin has obvious inhibitory effect on humoral immunity, promoting effect on cellular immunity, and may have immune regulation effect. . Intramuscular artemether also significantly inhibited T, B, Tu and tr lymphocytes in peripheral blood of begle rats. It also significantly decreased the serum IgG content and increased the spleen weight of normal mice. Reduce the serum IgG content of chicken red blood cell sensitized mice. Intravenous injection of artemisinin 50-100mg / kg significantly increased the phagocytic rate (50.2-53.1%) and phagocytic index (1.58-1.91) of peritoneal macrophages in mice. Artemisinin can also improve lymphocyte transformation rate and promote cellular immunity. Artesunate can promote the proliferation of TS cells, inhibit the production of te cells, and prevent the release of interleukin and various inflammatory mediators, thus playing an immunomodulatory role.
6. effects on the cardiovascular system: rabbit heart perfusion showed that artemisinin can slow down heart rate, inhibit myocardial contractility, and reduce coronary flow. Intravenous injection can reduce blood pressure, but does not affect the pressor response of norepinephrine. It is believed that the main reason is the direct inhibition of the heart. Artemisinin 20mg / kg intravenously can inhibit aconitine induced arrhythmia in rabbits.
. Artemisinin has obvious curative effect on experimental silicosis. Artemether has radioprotective effect on mice.